| 摘要 |
A pharmaceutically-active polymeric compound of the general formula (I), <?in-line-formulae description="In-line Formulae" end="lead"?>Y-[Y<SUB>n</SUB>-LINK B-X]<SUB>m</SUB>-LINK B (I) <?in-line-formulae description="In-line Formulae" end="tail"?> wherein (i) X is a coupled biological coupling agent of the general formula (II) <?in-line-formulae description="In-line Formulae" end="lead"?>Bio-LINK A-Bio (II) <?in-line-formulae description="In-line Formulae" end="tail"?> wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond; and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; (ii) Y is LINK B-OLIGO; wherein (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units; (iii) m is 1-40; and (iv) n is selected from 2-50. The compounds are useful as biomaterials, particularly, providing antibacterial a.i. in vivo. Also provided are biological coupling agents useful as intermediates in the preparation of the pharmaceutically-active polymeric compounds.
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